Solid Oral Modified Release Dosage Forms

Question 1

What is the Goal of DDS?

Answer 1

Provide a therapeutic amount of drug to a proper site so the desired drug concentration is achieved promptly, then maintained

Question 2

An important aspect of DDS which targets drugs to specific organs, tissue, cells, or subcellular compartments

Answer 2

Spatial placement

Question 3

An aspect of DDS that controls the rate of drug delivery to the target site

Answer 3

Temporal Delivery

Question 4

Products that are enteric-coated tablets or capsules designed to pass through the stomach unaltered → later release of medication in the intestinal tract

Answer 4

Delayed release products

Question 5

Products that designed to release their medication in a controlled manner, at a predetermined rate, duration, and location to achieve and maintain optimum therapeutic blood levels of drug

Answer 5

Extended - Release Products

Question 6

BSC Class most suitable for extended - release delivery

Answer 6

BCS Class 1

Question 7

BCS class that is most challenging to formulate as modified - release products

Answer 7

Class IV drugs

Question 8

Why is there a need for extended release drugs?

Answer 8

+ Multiple dosing is inconvenient: missed doses, made-up dose, noncompliance
+ Too frequent intake: MTC reached with toxic side efx
+ Missed doses: subtherapeutic levels

Question 9

Disadvantages of ER Dosage forms

Answer 9

+ Loss of Dose Flexibility
+ Dose Dumping

Question 10

a general term used to describe dosage forms having drug-release features based on time, course, and/or location that are designed to accomplish therapeutic or convenience objectives not offered by conventional or immediate- release form

Answer 10

Modified - Release

Question 11

Modified - release example that allows a reduction in dosing frequency from that necessitated
by a conventional dosage form

Answer 11

Extended Release

Question 12

Designed to release the drug at a time other than promptly after
administration

Answer 12

Delayed - Release

Question 13

Enteric Coating materials

Answer 13

Fats
Fatty Acids
Waxes
Shellac
Cellulose Acetate Phthalates

Question 14

Type of Delayed Release Mechanism that:

• Protect the drug in the dosage form from the harmful effects of the gastric environment
• Minimize the irritating effects of certain drugs (e.g., nonsteroidal anti-inflammatory drugs) on the gastric mucosa
• Deliver the drug to the intestine for local effects.

Answer 14

Gastro-resistant coatings

Question 15

Coatings that respond to enzymatic breakdown are now being considered as
protective coatings suitable for the colonic delivery of polypeptide drugs

Answer 15

Colonic Drug Delivery

Question 16

Modified release mechanism that contains two single doses of medications, one for immediate release (first dose) and the second for delayed release (second dose)

Answer 16

Repeat Action

Question 17

Described drug release directed toward isolating or concentrating a drug in a body region, tissue, or site for absorption or for drug action

Answer 17

Targeted Release

Question 18

True/False:

A. Drugs absorbed slowly are naturally short acting.
B. Drugs with short t1/2 (< 2h) are poor candidates; may require large quantities

Answer 18

False, Naturally Long Acting
True.

Question 19

Characteristic of Extended Release Products where the drug has a good margin of safety

Answer 19

WIde therapeutic index

Question 20

Microcrystalline spheres are more durable than other nonpareil seeds.

Answer 20

True

Question 21

Coating Lipids in ER Technologies

Answer 21

Beeswax
Carnauba Wax
Glyceryl Monostearate
Cetyl Alcohol
Ethylcellulose

Question 22

ER Tech. Compressed tablets (8 – 10 minitablets) are placed in a gelatin capsule

Answer 22

Multitablet system

Question 23

Enclosing materials in a wall forming material leading to coacervation (i.e. gelatin)

Answer 23

Microencapsulated Drug

Question 24

Examples of Wall Forming Material in Microencapsulated Drugs

Answer 24

Gelatin
Polyvinyl Alchohol
Ethylcellulose
Polyvinyl chloride

Question 25

The primary mechanism of drug release occurs when the polymer swells on contact with the aqueous medium to form a gel layer on the surface of the system

Answer 25

Embedding drug in slowly eroding or hydrophilic matrix system

Question 26

Drug is released from the matrix by diffusion wherein the plastic form retains its shape during its passage through the alimentary tract

Answer 26

Embedding drug in inert plastic matrix

Question 27

release the drug in a controlled manner to their specific site of action - retains on the targeted site

Answer 27

Gastroretention forms i.e. tx of H.pylori

Question 28

An Active (drug) and push (polymeric osmotic agent) layers, operating with the principle of osmotic pressure

Answer 28

Osmotic pump

Question 29

What factors are not affecting osmotic pump?

Answer 29

Gastrointestinal acidity
Alkalinity
Fed Conditions
Gastrointestinal motility

Question 30

Example of Osmotic Pump

Answer 30

Adalat 30

Question 31

Initial dose (outer shell or coating) of the drug is released
immediately and a second dose (inner core) is released later

Answer 31

Repeat Action Tablets

Question 32

T/F. It is normal to find empty shells or ghosts from osmotic tablets in the stool.

Answer 32

True